Aurones as histone deacetylase inhibitors: identification of key features

Date

2014

Authors

Zwick, V.
Chatzivasileiou, A.-O.
Deschamps, N.
Roussaki, M.
Simões-Pires, C.A.
Nurisso, A.
Denis, I.
Blanquart, C.
Martinet, N.
Carrupt, P.-A.

Editors

Advisors

Journal Title

Journal ISSN

Volume Title

Type:

Journal article

Citation

Bioorganic and Medicinal Chemistry Letters, 2014; 24(23):5497-5501

Statement of Responsibility

Vincent Zwick, Alkiviadis-Orfefs Chatzivasileiou, Nathalie Deschamps, Marina Roussaki, Claudia A. Simões-Pires ... Iza Denis ... et al.

Conference Name

DOI

10.1016/j.bmcl.2014.10.019

Abstract

In this study, a total of 22 flavonoids were tested for their HDAC inhibitory activity using fluorimetric and BRET-based assays. Four aurones were found to be active in both assays and showed IC50 values below 20 μM in the enzymatic assay. Molecular modelling revealed that the presence of hydroxyl groups was responsible for good compound orientation within the isoenzyme catalytic site and zinc chelation.

School/Discipline

Dissertation Note

Provenance

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Rights

© 2014 Elsevier Ltd. All rights reserved.

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Published Version

https://doi.org/10.1016/j.bmcl.2014.10.019

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Persistent link to this record

http://hdl.handle.net/2440/118656